TRV-120027 praglurant 5R)-5-((sulfamoylamino)methyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3

5R)-5-((sulfamoylamino)methyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3

20(8): 942-947

Pharmacokinetic dose-scheduling study of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors

used as positive controls

39(2):319-25

TRV-120027 praglurant 5R)-5-((sulfamoylamino)methyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3TRV120027, a arrestin 1 biased agonist of the angiotensin II receptor type 1 (AT1R), engages arrestins while blocking G protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R arrestin 1TRPC3PLC at the plasma membrane. TRV120027 inhibits angiotensin IImediated vasoconstriction and increases cardiomyocyte contractility.